Compounds, compositions, and methods for treatment of disease
A compound and an independent technology, applied in the direction of chemical instruments and methods, drug combinations, active ingredients of heterocyclic compounds, etc., can solve problems such as autoinflammatory disorders
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[0340] The invention now generally described may be more readily understood by reference to the following examples, which are included for the purpose of illustrating certain aspects and embodiments of the invention only and are not intended to be limiting of the invention.
example 1
[0341] Example 1: Preparation of Exemplary Compounds of the Disclosure
[0342] method 1:
[0343]
[0344] To a solution of an appropriately substituted purine (2 mmol) and RBr / RCl / RI (2.5 mmol) in anhydrous DMF (5 mL) was added anhydrous potassium carbonate (3 mmol) and a few crystals of NaI. The suspension was heated slowly under argon in an oil bath at 65°C-70°C for 3h. The progress of the reaction was monitored on TLC using DCM-MeOH (2.5%). After the reaction was complete, the reaction mixture was cooled to room temperature and concentrated at 50 °C to remove most of the DMF. Hexanes (10 mL) were added and the remaining DMF was removed. The residue was partitioned between EtOAc (50 mL) and water (15 mL). The organic layer was separated, and the aqueous layer was re-extracted into EtOAc (25 mL). The combined organic layers were washed with water (15ml), sodium bicarbonate (5%, 2X 15mL) and then with saturated NaCl solution (10mL). The organic layer was washed ...
example 2
[0934] Example 2: Protocol for Testing STING Antagonistic Activity of Exemplary Compounds of the Disclosure in THP-1 and RAW Cells
[0935] Cells and Cell Culture Conditions
[0936] THP-1 double cells (InvivoGen) were incubated at 37°C in 5% CO 2 cultured in RPMI containing 10% fetal bovine serum (FBS), 100 IU mL-1 penicillin and 100 μg mL-1 streptomycin. RAW-ISG cells (InvivoGen) were incubated at 37 °C in 5% CO 2 cultured in DMEM containing 10% fetal bovine serum (FBS), 100 IU mL-1 penicillin and 100 μg mL-1 streptomycin. THP-1 double cells were seeded into 96-well assay plates on the day of the assay, while RAW cells were seeded into 96-well assay plates 18 hours before the assay.
[0937] Cell-based ISG54 promoter-reporter luciferase measurement of IRF activity in THP-1 double cells:
[0938] 50,000 cells seeded in 96-well flat-bottomed white assay plates were treated with compounds at different concentrations (10uM to 0.01uM) for 1 h, and then STING was induced wit...
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